Journal
TETRAHEDRON LETTERS
Volume 63, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2020.152719
Keywords
Amidation; Amines; Carboxylic acids; EDC; HOBt; DMAP
Categories
Funding
- National Institutes of Health [AI150466]
- Purdue University Center for Cancer Research
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The study presents a convenient protocol for amide bond formation, suitable for electron deficient amines and carboxylic acids, enabling the synthesis of a variety of functionalized amide derivatives.
A convenient protocol for amide bond formation for electron deficient amines and carboxylic acids is described. Amide coupling of aniline derivatives has been investigated with a number of reagents under a variety of reaction conditions. The use of 1 equivalent of EDC and 1 equivalent of DMAP, catalytic amount of HOBt and DIPEA provided the best results. This method is applicable for the synthesis of a range of functionalized amide derivatives with electron deficient and unreactive amines. (C) 2020 Elsevier Ltd. All rights reserved.
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